Ramsay L, Asbury M, Shelton J, Harrison I
Clin Pharmacol Ther. 1977 May;21(5):602-9. doi: 10.1002/cpt1977215602.
Relative dose ratios of the mineralocorticoid antagonists spironolactone (100 mg and 200 mg daily) and canrenoate-K (200 mg daily) at steady state were defined in six healthy subjects with fludrecortisone as the mineralocorticoid agonist. The urine log 10 Na/K responses during spironolactone treatments were consistent with the law of mass action. The potency of canrenoate-K was 0.68 (95% C.L. 0.53 to 0.89) that of spironolactone on a weight basis. Approximately 72% of the renal antimineralocorticoid activity of spironolactone could attributed to the metabolite canrenone. The results at steady state are contrasted with those of a previously study comparing single doses of spironolactone and canrenoate-K.
在6名健康受试者中,以氟氢可的松作为盐皮质激素激动剂,确定了盐皮质激素拮抗剂螺内酯(每日100毫克和200毫克)和坎利酸钾(每日200毫克)在稳态时的相对剂量比。螺内酯治疗期间尿中log10钠/钾反应符合质量作用定律。以重量计,坎利酸钾的效力为螺内酯的0.68(95%置信区间为0.53至0.89)。螺内酯约72%的肾脏抗盐皮质激素活性可归因于代谢产物坎利酮。将稳态时的结果与先前比较单次剂量螺内酯和坎利酸钾的研究结果进行了对比。